Nintedanib esylate

This product is for research use only, not for human use. We do not sell to patients.

Nintedanib esylate
For small sizes, please check our retail website as below: www.invivochem.com
Size Price Stock
1g$700In Stock
5g$1800In Stock
10g$2700In Stock

Cat #: V10056 CAS #: 656247-18-6 Purity ≥ 98%

Description: Nintedanib esylate (formerly also known as BIBF 1120 esylate; BIBF-1120 esylate; Vargatef), the esylate salt of nintedanib, is a novel, orally bioavailable, potent triple angiokinase inhibitor that has gained FDA approval in 2014 for the treatment of idiopathic pulmonary fibrosis (IPF).

References: Hilberg F, et al. BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res, 2008, 68(12), 4774-4782.

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Molecular Weight (MW)649.76
Molecular FormulaC33H39N5O7S
CAS No.656247-18-6
SMILES Code O=C(C1=CC(NC/2=O)=C(C=C1)C2=C(NC3=CC=C(N(C)C(CN4CCN(C)CC4)=O)C=C3)/C5=CC=CC=C5)OC.CCS(=O)(O)=O
SynonymsBIBF1120; BIBF 1120 BIBF-1120; Nintedanib esylate. Nintedanib ethanesulfonate salt; Intedanib; Brand name OFEV. Vargatef
ProtocolIn VitroNintedanib (BIBF 1120) binds to the ATP-binding site in the cleft between the amino and carboxy terminal lobes of the kinase domain. Nintedanib (BIBF 1120) inhibits proliferation of PDGF-BB stimulated BRPs with EC50 of 79 nM in cell assays. Nintedanib (BIBF 1120) (100 nM) blocks activation of MAPK after stimulation with 5% serum plus PDGF-BB. Nintedanib (BIBF 1120) prevents PDGF-BB stimulated proliferation with an EC50 of 69 nM in cultures of human vascular smooth muscle cells (HUASMC).
In VivoNintedanib (BIBF 1120) (25-100 mg/kg daily p.o.) is highly active in all tumor models, including human tumor xenografts growing in nude mice and a syngeneic rat tumor model. This is evident in the magnetic resonance imaging of tumor perfusion after 3 days, reducing vessel density and vessel integrity after 5 days, and profound growth inhibition.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM1.5390 mL7.6951 mL15.3903 mL30.7806 mL
5mM0.3078 mL1.5390 mL3.0781 mL6.1561 mL
10mM0.1539 mL0.7695 mL1.5390 mL3.0781 mL
20mM0.0770 mL0.3848 mL0.7695 mL1.5390 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
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Volume
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Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.